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Target
TGF-beta receptor type-1 [T204D]
Ligand
BDBM283007
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
0.700±n/a nM
Citation
 Kinsella, T; Gelman, M; Hong, H; Darwish, IS; Singh, R; Yu, J; Borzilleri, RM; Velaparthi, U; Liu, P; Darne, CP; Rahaman, H; Warrier, JS TGF-β inhibitors US Patent  US10287295 Publication Date 5/14/2019 
Target
Name:
TGF-beta receptor type-1 [T204D]
Synonyms:
ALK5 | SKR4 | TGF-beta receptor type-1 (T204D) | TGF-betaR1 T204D | TGFBR1 | TGFBR1T204D | TGFR-1 (T204D) | TGFR1_HUMAN
Type:
n/a
Mol. Mass.:
55981.22
Organism:
Homo sapiens (Human)
Description:
P36897[T204D]
Residue:
503
Sequence:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARDIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM283007
Synonyms:
6-(1-(2,2-difluoroethyl)-4-(4-fluorophenyl)-1H- imidazol-5-yl)-N-methoxyimidazo[1,2-b]pyridazine-3- carboxamide | US10287295, Example 209' | US11352360, Example 209' | US9884868, Example 209'
Type:
Small organic molecule
Emp. Form.:
C19H15F3N6O2
Mol. Mass.:
416.3566
SMILES:
CONC(=O)c1cnc2ccc(nn12)-c1c(ncn1CC(F)F)-c1ccc(F)cc1
Structure:
Search PDB for entries with ligand similarity: